Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 4, Pages 639-643Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.8b00608
Keywords
Chalcone; tetrahydronaphthalene scaffold; Notch inhibitors; T-ALL; cancer
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Funding
- COST Action [CM1407]
- Universidad del Valle (CIAM-2017)
- Science, Technology and Innovation Fund General Royalties System (FCTeI-SGR) [BPIN 2013000100007]
- Italian Ministry of Education, University and Research - Dipartimenti di Eccellenza [L. 232/2016]
- MINECO/FEDER [SAF2015-64629-C2-1-R]
- MIUR PNR 2015-2020 [ARS01_00432]
- Sapienza University [RG116154E2-C7A6FB]
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Based on hit-likeness and chemical diversity, a number of chalcones and chalcone-mimetic compounds were selected as putative Notch inhibitors. The evaluation of the antiproliferative effect combined with the inhibition of Notchl expression in KOPTK1 cell line identified compound 18, featuring a tetrahydronaphthalene-based scaffold, as a new promising Notch-blocking agent.
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